Lesinurad (Synonyms: RDEA594)

Name: Lesinurad
Brand: MedChemExpress
SKU: HY-15258
Rating: 5.0 (2 reviews)

Cat. No.: HY-15258 Purity: 99.96%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

Lesinurad is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with K_m values of 0.85 and 2 µM, respectively.

For research use only. We do not sell to patients.

Lesinurad Chemical Structure

CAS No. : 878672-00-5

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 33	In-stock	Estimated Time of Arrival: December 31
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10 mM * 1 mL in DMSO	USD 33	In-stock	Estimated Time of Arrival: December 31
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5 mg	USD 30	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 50	In-stock	Estimated Time of Arrival: December 31
25 mg	USD 103	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 166	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 267	In-stock	Estimated Time of Arrival: December 31
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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Lesinurad:

Lesinurad sodium In-stock

2 Publications Citing Use of MCE Lesinurad

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Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

Lesinurad is a URAT1 and OAT inhibitor, is determined to be a substrate for the kidney transporters OAT1 and OAT3 with K_m values of 0.85 and 2 µM, respectively.

IC₅₀ & Target

Km: 0.85 µM (OAT1), 2 µM (OAT3)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	15.1 μM Compound: (-)-lesinurad	Inhibition of human URAT1 expressed in HEK293 cells assessed as inhibition of [14C]uric acid uptake preincubated for 15 mins followed by [14C]uric acid addition measured after 10 mins by liquid scintillation counting method Inhibition of human URAT1 expressed in HEK293 cells assessed as inhibition of [14C]uric acid uptake preincubated for 15 mins followed by [14C]uric acid addition measured after 10 mins by liquid scintillation counting method	[PMID: 28337320]
HEK293	IC₅₀	2.03 μM Compound: 12	Inhibition of human OAT4 expressed in HEK293 cells by assessed as [14C]urate uptake preincubated for 5 mins followed by [14C]urate addition and measured after 10 mins by liquid scintillation counting method Inhibition of human OAT4 expressed in HEK293 cells by assessed as [14C]urate uptake preincubated for 5 mins followed by [14C]urate addition and measured after 10 mins by liquid scintillation counting method	[PMID: 31774679]
HEK293	IC₅₀	4.4 μM Compound: (+)-lesinurad	Inhibition of human URAT1 expressed in HEK293 cells assessed as inhibition of [14C]uric acid uptake preincubated for 15 mins followed by [14C]uric acid addition measured after 10 mins by liquid scintillation counting method Inhibition of human URAT1 expressed in HEK293 cells assessed as inhibition of [14C]uric acid uptake preincubated for 15 mins followed by [14C]uric acid addition measured after 10 mins by liquid scintillation counting method	[PMID: 28337320]
HEK293	IC₅₀	7.3 μM Compound: (+/-)-Lesinurad	Inhibition of human URAT1 expressed in HEK293 cells assessed as inhibition of [14C]uric acid uptake preincubated for 15 mins followed by [14C]uric acid addition measured after 10 mins by liquid scintillation counting method Inhibition of human URAT1 expressed in HEK293 cells assessed as inhibition of [14C]uric acid uptake preincubated for 15 mins followed by [14C]uric acid addition measured after 10 mins by liquid scintillation counting method	[PMID: 28337320]

In Vitro

Lesinurad is a novel selective uric acid reabsorption inhibitor (SURI). Lesinurad is determined to be a substrate for the kidney transporters organic anion transporter (OAT1) and OAT3 with K_m values of 0.85 and 2 μM, respectively^[1]. Lesinurad (RDEA594) is a URAT1 and OAT inhibitor, which increases proximal renal tubule urate excretion^[2]. Lesinurad (RDEA594) is a potential uric acid lowering agent througn inhibition of uric acid reuptake, and exhibits favorable p450 profiles, inhibits CYP2C9 and CYP2C8 with IC₅₀ of 14.4 μM and 16.2 μM, respectively. IC₅₀s of Lesinurad are all above 100 μM for CYP1A2, CYP2C19,and CYP2D6^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Lesinurad (RDEA594) shows better pharmacokinetics than its pro-drug RDEA806. The 100 mg dose of Lesinurad exhibits a phamacological effect in the range of that produced by 300 mg to 800 mg single doses of RDEA806^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

Molecular Weight

404.28

Formula

C₁₇H₁₄BrN₃O₂S

CAS No.

878672-00-5

Appearance

Solid

Color

White to off-white

SMILES

BrC1=NN=C(SCC(O)=O)N1C2=C3C(C=CC=C3)=C(C4CC4)C=C2

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (247.35 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.4735 mL	12.3677 mL	24.7353 mL
5 mM	0.4947 mL	2.4735 mL	4.9471 mL
10 mM	0.2474 mL	1.2368 mL	2.4735 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (6.18 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.96%

Select Batch:

Data Sheet (284 KB) SDS (393 KB)

COA (256 KB) HNMR (180 KB) RP-HPLC (344 KB)

Handling Instructions (2659 KB)

References

[1]. Shen Z, et al. In Vitro and In Vivo Interaction Studies Between Lesinurad, a Selective Urate Reabsorption Inhibitor, and Major Liver or Kidney Transporters. Clin Drug Investig. 2016 Jun;36(6):443-52 [Content Brief]

[2]. Sattui SE, et al. Treatment of hyperuricemia in gout: current therapeutic options, latest developments and clinical implications. Ther Adv Musculoskelet Dis. 2016 Aug;8(4):145-59. [Content Brief]

[3]. L.Yeh, et al. RDEA594, a potential uric acid lowering agent througn inhibition of uric acid reuptake ,shows better pharmacokinetics rhan its prodrug RDEA806. 2008 ACR/ARHP Annual Scientific Meeting, 24-29 October 2008, USA.

Cell Assay
^[1]

Validated oocytes, HEK293, MDCK-II, Caco-2 or MDCK-MDR1 cell systems are used to study the interaction of Lesinurad with membrane transporters localized to the kidney (OAT1, OAT3, OCT2, MATE1, and MATE2K) or liver (P-gp, BCRP, OATP1B1, OATP1B3, and OCT1). Xenopus laevis oocytes are injected with OAT1 or OAT3 cRNA or control (water) while HEK293 cells are stably transfected with MATE1, MATE2K, or vector and MDCK-II cells with hOATP1B1, hOATP1B3, hOCT1, hOCT2, or vector. The MDCKII cell line is stably transfected with the human MDR1 gene to create a P-gp cell line. The interaction of Lesinurad with BCRP relied on the endogenous expression in Caco-2 cells. All cells are cultured with growth medium according to standard methodology. In order to determine whether Lesinurad is a substrate for a transporter, cells are incubated with [¹⁴C]-labeled Lesinurad at various concentrations and the amount of Lesinurad taken up by the cells determined by subtracting the uptake in vector cells from that in the transfected cells. The uptake of a [³H]-labeled known substrate of the transporter served as the positive control. Inhibition of a transporter by Lesinurad is determined by incubating cells with a fixed concentration of [³H]-labeled known substrate and various concentrations of unlabeled Lesinurad. Inhibition by a known inhibitor of each transporter served as the positive control. Cells are incubated for the appropriate amount of time. All reactions are terminated by the addition of ice-cold medium. The cells are then rinsed with medium and lysed^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

[1]. Shen Z, et al. In Vitro and In Vivo Interaction Studies Between Lesinurad, a Selective Urate Reabsorption Inhibitor, and Major Liver or Kidney Transporters. Clin Drug Investig. 2016 Jun;36(6):443-52 [Content Brief]

[2]. Sattui SE, et al. Treatment of hyperuricemia in gout: current therapeutic options, latest developments and clinical implications. Ther Adv Musculoskelet Dis. 2016 Aug;8(4):145-59. [Content Brief]

[3]. L.Yeh, et al. RDEA594, a potential uric acid lowering agent througn inhibition of uric acid reuptake ,shows better pharmacokinetics rhan its prodrug RDEA806. 2008 ACR/ARHP Annual Scientific Meeting, 24-29 October 2008, USA.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.4735 mL	12.3677 mL	24.7353 mL	61.8383 mL
	5 mM	0.4947 mL	2.4735 mL	4.9471 mL	12.3677 mL
	10 mM	0.2474 mL	1.2368 mL	2.4735 mL	6.1838 mL
	15 mM	0.1649 mL	0.8245 mL	1.6490 mL	4.1226 mL
	20 mM	0.1237 mL	0.6184 mL	1.2368 mL	3.0919 mL
	25 mM	0.0989 mL	0.4947 mL	0.9894 mL	2.4735 mL
	30 mM	0.0825 mL	0.4123 mL	0.8245 mL	2.0613 mL
	40 mM	0.0618 mL	0.3092 mL	0.6184 mL	1.5460 mL
	50 mM	0.0495 mL	0.2474 mL	0.4947 mL	1.2368 mL
	60 mM	0.0412 mL	0.2061 mL	0.4123 mL	1.0306 mL
	80 mM	0.0309 mL	0.1546 mL	0.3092 mL	0.7730 mL
	100 mM	0.0247 mL	0.1237 mL	0.2474 mL	0.6184 mL

Lesinurad Related Classifications

Metabolic Disease

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Lesinurad878672-00-5RDEA594RDEA 594RDEA-594OATURAT1Organic anion transporterUrate transporter 1SLC22A12Inhibitorinhibitorinhibit

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Lesinurad (Synonyms: RDEA594)

Customer Review

Other Forms of Lesinurad:

Lesinurad Related Antibodies

2 Publications Citing Use of MCE Lesinurad

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Lesinurad Related Antibodies

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Complete Stock Solution Preparation Table

Lesinurad Related Classifications

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